Apalutamide
Based on 15 publication(s) in Google Scholar
Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
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- Purity: 99.94%
- CAS No.: 956104-40-8
- 화학식: C21H15F4N5O2S
- 분자량:477.43
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Apalutamide
More- Cell Death Dis. 2021 Jul 27;12(8):740. [Abstract]
- NPJ Breast Cancer. 2026 Feb 24. [Abstract]
- Br J Cancer. 2022 Sep;127(5):927-936. [Abstract]
- JCI Insight. 2019 Sep 5;4(17):e122688. [Abstract]
- Biosensors (Basel). 2024 Apr 5;14(4):175. [Abstract]
- Mol Cancer Ther. 2016 Jul;15(7):1702-12. [Abstract]
- Chem Biol Interact. 2024 Jan 25:388:110840. [Abstract]
- Front Pharmacol. 2021 Jul 19:12:720387. [Abstract]
- Mol Cancer Res. 2017 Jan;15(1):35-44. [Abstract]
- Drug Metab Dispos. 2025 Apr;53(4):100052. [Abstract]
- Aging (Albany NY). 2024 Apr 19;16(8):7249-7266. [Abstract]
- Sci Rep. 2019 Sep 24;9(1):13786. [Abstract]
- Arch Biochem Biophys. 2023 Feb:735:109519. [Abstract]
- Prostate. 2025 Sep 19. [Abstract]
- Biomed Chromatogr. 2026 Mar;40(3):e70376. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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Histological Imaging/Staining
Biological Activity
IC50: 16 nM (Androgen receptor)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-7 | CC50 |
>50 μM
Compound: ARN-509
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Antiproliferative activity against African green monkey COS-7 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method
Antiproliferative activity against African green monkey COS-7 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method
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[PMID: 38385428] |
| CWR22R | CC50 |
>50 μM
Compound: ARN-509
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Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method
Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method
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[PMID: 38385428] |
| DU-145 | CC50 |
>50 μM
Compound: ARN-509
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Antiproliferative activity against human DU-145 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method
Antiproliferative activity against human DU-145 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method
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[PMID: 38385428] |
| HEK293 | IC50 |
0.016 μM
Compound: 6
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Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of R1881-induced receptor transactivation after 24 hrs by luciferase reporter gene assay
Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of R1881-induced receptor transactivation after 24 hrs by luciferase reporter gene assay
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[PMID: 30525603] |
| LNCaP | CC50 |
9.72 μM
Compound: ARN-509
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Antiproliferative activity against human LNCaP cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method
Antiproliferative activity against human LNCaP cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method
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[PMID: 38385428] |
| LNCaP | IC50 |
174 nM
Compound: 5, ARN-509
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Antiproliferative activity against human LNCAP cells after 3 days
Antiproliferative activity against human LNCAP cells after 3 days
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[PMID: 26046313] |
| LNCaP C4-2 | CC50 |
41.67 μM
Compound: ARN-509
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Antiproliferative activity against human C4-2 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method
Antiproliferative activity against human C4-2 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method
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[PMID: 38385428] |
| PC-3 | CC50 |
>50 μM
Compound: ARN-509
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Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method
Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method
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[PMID: 38385428] |
Apalutamide (ARN-509) also exhibits low micromolar affinity (IC50 3 μM) for the GABAA receptor in radioligand binding-assays and thus may potentially antagonize GABAA at therapeutic dose levels[1]. Apalutamide is a potent androgen receptor (AR) antagonist that targets the AR ligand-binding domain and prevents AR nuclear translocation, DNA binding, and transcription of AR gene targets[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 956104-40-8
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Appearance Solid
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분자량 477.43
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화학식 C21H15F4N5O2S
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Color White to off-white
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SMILES
O=C(NC)C1=CC=C(N(C(N(C2=CC(C(F)(F)F)=C(C#N)N=C2)C3=O)=S)C43CCC4)C=C1F
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Synonyms
ARN-509
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (15)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
2021 Jul 27;12(8):740. PMID: 34315855
Apalutamide purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2021 Jul 27;12(8):740. [Abstract]
PCa cells were treated with the AR antagonist Apalutamide (Apa) (25 µM) in the colony formation assay.
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NPJ Breast Cancer
Transcriptomic analysis to uncover the mechanism of radiosensitization of AR-positive triple-negative breast cancers with AR inhibition. [Abstract]2026 Feb 24. PMID: 41735341
Apalutamide purchased from MedChemExpress. Usage Cited in: NPJ Breast Cancer. 2026 Feb 24. [Abstract]
Apalutamide (ARN-509) (500 nM-2 μM; 1 h) radiosensitized AR+ TNBC MDA-MB-453 cells.
Apalutamide purchased from MedChemExpress. Usage Cited in: NPJ Breast Cancer. 2026 Feb 24. [Abstract]
Clonogenic survival assay curves and radiation enhancement ratios (rER) with Apalutamide (ARN-509) (5 µM) of both sham transfected and ERK-overexpressing ACC-422 cells.
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Br J Cancer
Androgen and oestrogen receptor co-expression determines the efficacy of hormone receptor-mediated radiosensitisation in breast cancer. [Abstract]2022 Sep;127(5):927-936. PMID: 35618789 -
JCI Insight
Targeting castration-resistant prostate cancer with androgen receptor antisense oligonucleotide therapy. [Abstract]2019 Sep 5;4(17):e122688. PMID: 31484823
Apalutamide purchased from MedChemExpress. Usage Cited in: JCI Insight. 2019 Sep 5;4(17):e122688. [Abstract]
Apalutamide (Apa) (30 mg/kg; once daily for 4 weeks). Plots of mean ± SEM of GUT and prostate weights of Pten-KO mice normalized to baseline means, and a waterfall plot of individual treatment response based on prostate tumor weight normalized to median baseline level.
Apalutamide purchased from MedChemExpress. Usage Cited in: JCI Insight. 2019 Sep 5;4(17):e122688. [Abstract]
Apalutamide (Apa) (30 mg/kg; once daily for 4 weeks). Representative images of whole genitourinary tracts and H&E-stained sections of dorsal prostate (DP) and ventral prostate (VP) tumors in Pten-KO mice.
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Biosensors (Basel)
An Extracellular Matrix Overlay Model for Bioluminescence Microscopy to Measure Single-Cell Heterogeneous Responses to Antiandrogens in Prostate Cancer Cells. [Abstract]2024 Apr 5;14(4):175. PMID: 38667168 -
Mol Cancer Ther
2016 Jul;15(7):1702-12. PMID: 27196756 -
Chem Biol Interact
Inhibition of aldo-keto reductase 1C3 overcomes gemcitabine/cisplatin resistance in bladder cancer. [Abstract]2024 Jan 25:388:110840. PMID: 38122923 -
Front Pharmacol
Icariin Ameliorates Diabetic Renal Tubulointerstitial Fibrosis by Restoring Autophagy via Regulation of the miR-192-5p/GLP-1R Pathway. [Abstract]2021 Jul 19:12:720387. PMID: 34349660 -
Mol Cancer Res
Exploitation of Castration-Resistant Prostate Cancer Transcription Factor Dependencies by the Novel BET Inhibitor ABBV-075. [Abstract]2017 Jan;15(1):35-44. PMID: 27707886 -
Drug Metab Dispos
Quantitative clinical risk assessment of CYP2C, UDP-glucuronosyltransferase, P-glycoprotein induction, and complex drug-drug interactions using TruVivo human hepatocyte triculture platform. [Abstract]2025 Apr;53(4):100052. PMID: 40133023 -
Aging (Albany NY)
AAT resistance-related AC007405.2 and AL354989.1 as novel diagnostic and prognostic markers in prostate cancer. [Abstract]2024 Apr 19;16(8):7249-7266. PMID: 38643469 -
Sci Rep
2019 Sep 24;9(1):13786. PMID: 31551480 -
Arch Biochem Biophys
Artepillin C overcomes apalutamide resistance through blocking androgen signaling in prostate cancer cells. [Abstract]2023 Feb:735:109519. PMID: 36642262 -
Prostate
MIF Facilitates Resistance to Androgen Deprivation Therapy by Regulating AMPD2 Expression in Prostate Cancer Cells. [Abstract]2025 Sep 19. PMID: 40968720 -
Biomed Chromatogr
Assessment of Apalutamide Metabolic Stability in HLMs Matrix Using a Sensitive and Fast UPLC-MS/MS Method: In Silico Screening for Toxicity Alerts and Metabolic Lability. [Abstract]2026 Mar;40(3):e70376. PMID: 41582395
용액&용해도
DMSO : 50 mg/mL (104.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.36 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Trypsinized VCaP cells are adjusted to a concentration of 100,000 cells per mL in phenol-red-free RPMI 1640 (with 5% CSS), and dispensed in 16 µL aliquots into CellBIND 384 well plates. Cells are incubated for 48 hours, after which ligand is added in a 16 µL volume to the RPMI culture medium. For the antagonist mode assay, the ligands are diluted in culture medium also containing 30 pM R1881. After 7 days’ incubation, 16 µL of CellTiter-Glo Luminescent Cell Viability Assay is added and Relative Luminescence Units (RLUs) measured[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
In vivo xenograft experiments to determine anti-tumor response are carried out in SHO SCID male mice. Mice are orchiectomized under isoflorane anesthesia and are given 2-3 days to recover prior to tumor cell injection. LNCaP/AR(cs) cells are suspended in 50% RPMI, 50% Matrigel, and 5×106 cells/xenograft are injected in a volume of 100 μL. Animals are observed weekly until tumor growth is apparent. From 24 d post-injection, tumors are measured weekly, and after 40-60 days post-injection, animals are randomized into cohorts of equivalent mean (150-250 mm3) and range tumor burden. All compounds (e.g., Apalutamide, 30 mg/kg per day) are administered daily by oral gavage. Statistical analyses are performed using Graphpad Prism.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Clegg NJ, et al. ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Res. 2012 Mar 15;72(6):1494-503. [Content Brief]
[2]. Smith MR, et al. Phase 2 Study of the Safety and Antitumor Activity of Apalutamide (ARN-509), a Potent Androgen Receptor Antagonist, in the High-risk Nonmetastatic Castration-resistant Prostate Cancer Cohort. Eur Urol. 2016 May 6. pii: S0302-2838(16)30133 [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0945 mL | 10.4727 mL | 20.9455 mL | 52.3637 mL |
| 5 mM | 0.4189 mL | 2.0945 mL | 4.1891 mL | 10.4727 mL | |
| 10 mM | 0.2095 mL | 1.0473 mL | 2.0945 mL | 5.2364 mL | |
| 15 mM | 0.1396 mL | 0.6982 mL | 1.3964 mL | 3.4909 mL | |
| 20 mM | 0.1047 mL | 0.5236 mL | 1.0473 mL | 2.6182 mL | |
| 25 mM | 0.0838 mL | 0.4189 mL | 0.8378 mL | 2.0945 mL | |
| 30 mM | 0.0698 mL | 0.3491 mL | 0.6982 mL | 1.7455 mL | |
| 40 mM | 0.0524 mL | 0.2618 mL | 0.5236 mL | 1.3091 mL | |
| 50 mM | 0.0419 mL | 0.2095 mL | 0.4189 mL | 1.0473 mL | |
| 60 mM | 0.0349 mL | 0.1745 mL | 0.3491 mL | 0.8727 mL | |
| 80 mM | 0.0262 mL | 0.1309 mL | 0.2618 mL | 0.6545 mL | |
| 100 mM | 0.0209 mL | 0.1047 mL | 0.2095 mL | 0.5236 mL |
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